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PE20081362A1 - MORPHOLINO PYRIMIDINE DERIVATIVES AS INHIBITORS OF mTOR KINASE AND PI3K - Google Patents

MORPHOLINO PYRIMIDINE DERIVATIVES AS INHIBITORS OF mTOR KINASE AND PI3K

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Publication number
PE20081362A1
PE20081362A1 PE2007001151A PE2007001151A PE20081362A1 PE 20081362 A1 PE20081362 A1 PE 20081362A1 PE 2007001151 A PE2007001151 A PE 2007001151A PE 2007001151 A PE2007001151 A PE 2007001151A PE 20081362 A1 PE20081362 A1 PE 20081362A1
Authority
PE
Peru
Prior art keywords
inhibitors
phenyl
alkyl
mtor kinase
pi3k
Prior art date
Application number
PE2007001151A
Other languages
Spanish (es)
Inventor
Maurice Raymond Verschoyle Finlay
Kurt Gordon Pike
Jeffrey Morris
Original Assignee
Astrazeneca Ab
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38720451&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20081362(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB0616747A external-priority patent/GB0616747D0/en
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of PE20081362A1 publication Critical patent/PE20081362A1/en

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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE MORFOLINA PIRIMIDINA DE FORMULA (I), EN DONDE m ES DE 0 A 4; Y1 E Y2 SON INDEPENDIENTEMENTE N O CR8, CON LA CONDICION DE QUE UNO SEA N Y EL OTRO CR8; X ES UN LIGADOR SELECCIONADO ENTRE -CR4=CR5-, -NR4CR6R7-, -OCR6R7-, -SCR6R7-, -S(O)CR6R7-, ENTRE OTROS; R1 ES H, ALQUILO(C1-C6), ALQUENILO(C2-C6), CARBOCICLILO, ENTRE OTROS; R2 ES ALQUILO(C1-C6), CARBOCICLILO Y HETEROCICLILO SUSTITUIDO CON NR17CONR18R19, ENTRE OTROS; CADA R3 ES HALO, CIANO, NITRO, -R13, -OR13, SR13, SOR13, CO2R13, ENTRE OTROS; O R1 Y R4 JUNTOS CON EL ATOMO AL CUAL ESTAN UNIDOS FORMAN UN CARBOCICLILO O HETEROCICLILO. SON SELECCIONADOS: 1-ETIL-3-[4-[4-[(3S)-3-METILMORFOLIN-4-IL]-6-(METILSULFONILMETIL)PIRIMIDIN-2-IL)FENIL]UREA, 1-[4-[4-(METILSULFONILMETIL)-6-MORFOLIN-4-IL-PIRIMIDIN-2-IL]FENIL]-3-FENIL-UREA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS SON INHIBIDORES DE LA mTOR QUINASA Y/O UNA O MAS ENZIMAS PI3K (TAL COMO LAS DE CLASE Ia Y/O Ib) POR LO QUE SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS TAL COMO EL CANCERREFERS TO COMPOUNDS DERIVED FROM PYRIMIDINE MORPHOLINE OF FORMULA (I), WHERE m IS FROM 0 TO 4; Y1 AND Y2 ARE INDEPENDENTLY N OR CR8, ON THE CONDITION THAT ONE IS N AND THE OTHER CR8; X IS A BINDER SELECTED FROM -CR4 = CR5-, -NR4CR6R7-, -OCR6R7-, -SCR6R7-, -S (O) CR6R7-, AMONG OTHERS; R1 IS H, ALKYL (C1-C6), ALKYL (C2-C6), CARBOCYCLYL, AMONG OTHERS; R2 IS ALKYL (C1-C6), CARBOCYCLYL AND HETEROCICLYL SUBSTITUTED WITH NR17CONR18R19, AMONG OTHERS; EACH R3 IS HALO, CYANE, NITRO, -R13, -OR13, SR13, SOR13, CO2R13, AMONG OTHERS; OR R1 AND R4 TOGETHER WITH THE ATOM TO WHICH THEY ARE UNITED FORM A CARBOCICLILO OR HETEROCICLILO. THEY ARE SELECTED: 1-ETHYL-3- [4- [4 - [(3S) -3-METHYLMORPHOLIN-4-IL] -6- (METHYLSULFONYLMETHYL) PYRIMIDIN-2-IL) PHENYL] UREA, 1- [4- [ 4- (METHYLSULFONYLMETIL) -6-MORFOLIN-4-IL-PYRIMIDIN-2-IL] PHENYL] -3-PHENYL-UREA, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION AND A PREPARATION PROCEDURE. THESE COMPOUNDS ARE INHIBITORS OF mTOR KINASE AND / OR ONE OR MORE PI3K ENZYMES (SUCH AS CLASS Ia AND / OR Ib) SO THEY ARE USEFUL IN THE TREATMENT OF PROLIFERATIVE DISEASES SUCH AS CANCER

PE2007001151A 2006-08-24 2007-08-24 MORPHOLINO PYRIMIDINE DERIVATIVES AS INHIBITORS OF mTOR KINASE AND PI3K PE20081362A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0616747A GB0616747D0 (en) 2006-08-24 2006-08-24 Novel compounds
US94854407P 2007-07-09 2007-07-09

Publications (1)

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PE20081362A1 true PE20081362A1 (en) 2008-11-14

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ID=38720451

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007001151A PE20081362A1 (en) 2006-08-24 2007-08-24 MORPHOLINO PYRIMIDINE DERIVATIVES AS INHIBITORS OF mTOR KINASE AND PI3K

Country Status (16)

Country Link
US (1) US7750003B2 (en)
EP (1) EP2057140B1 (en)
JP (1) JP5534811B2 (en)
KR (1) KR101435231B1 (en)
AR (1) AR062526A1 (en)
AU (1) AU2007287428B2 (en)
CA (1) CA2660758A1 (en)
CL (1) CL2007002446A1 (en)
CO (1) CO6150160A2 (en)
HK (1) HK1130776A1 (en)
IL (1) IL196998A0 (en)
MX (1) MX2009002046A (en)
NO (1) NO20090631L (en)
PE (1) PE20081362A1 (en)
UY (1) UY30559A1 (en)
WO (1) WO2008023159A1 (en)

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